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ALX-430-155
Revised 16-Nov-07
4EGI-1
SYNONYMS
α-[2-[4-(3,4-Dichlorophenyl)-2-thiazolyl]hydrazinylidene]-2-nitro-benzenepropanoic acid
PRODUCT LINE
DNA Regulation / Transcription
PRODUCT CATEGORY
Translation Inhibitors
Ordering Information
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ALX-430-155-M002
2 mg
190.00 USD
Product Specification
FORMULA:
C
18
H
12
Cl
2
N
4
O
4
S
MW:
451.3
CAS NUMBER:
315706-13-9
PURITY:
≥95%
APPEARANCE:
Brown solid.
SOLUBILITY:
Soluble in DMSO.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Protect from light.
IDENTITY:
Determined by
1
H-NMR,
13
C-NMR and MS.
Product Description
Selective and cell permeable inhibitor of the interaction between the human eukaryotic translation initiation factors 4E (eIF4E) and 4G (eIF4G).
Product Specific Literature References
Small-molecule inhibition of the interaction between the translation initiation factors eIF4E and eIF4G:
N.J. Moerke, et al.; Cell
128
, 257 (2007)
Abstract
ALX-430-156
Revised 21-Apr-08
6BIO
SYNONYMS
(2’Z,3’E)-6-Bromoindirubin-3’-oxime
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
GSK-3 Inhibitors
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ALX-430-156-M001
1 mg
40.00 USD
Product Specification
FORMULA:
C
16
H
10
BrN
3
O
2
MW:
356.2
CAS NUMBER:
667463-62-9
PURITY:
≥98%
APPEARANCE:
Dark red solid.
SOLUBILITY:
Soluble in DMSO.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Protect from light.
HAZARD:
IRRITANT.
Product Description
Inhibitor of phosphoinositide-dependent kinase 1 (PDK1). Potent, reversible and ATP-competitive inhibitor of glycogen synthase kinase-3α/β (GSK-3α/β).
Product Specific Literature References
Structural basis for the synthesis of indirubins as potent and selective inhibitors of glycogen synthase kinase-3 and cyclin-dependent kinases:
P. Polychronopoulos, et al.; J. Med. Chem.
47
, 935 (2004)
Abstract
7-Bromoindirubin-3’-oxime induces caspase-independent cell death:
J. Ribas, et al.; Oncogene
25
, 6304 (2006)
Abstract
Inverse in silico screening for identification of kinase inhibitor targets:
S. Zahler, et al.; Chem. Biol.
14
, 1207 (2007)
Abstract
An integrated computational approach to the phenomenon of potent and selective inhibition of aurora kinases B and C by a series of 7-substituted indirubins:
V. Myrianthopoulos, et al.; J. Med. Chem.
50
, 4027 (2007)
Abstract
Related Products
ALX-270-271
Indirubin-3'-monoxime
ALX-430-149
7BIO
ALX-430-157
Me-7BIO
ALX-270-296
Indirubin-5-sulfonic acid . sodium salt
ALX-270-361
Indirubin
ALX-270-424
5-Iodo-indirubin-3'-monoxime
Further Categories Containing This Product:
PI(3)K-Akt-mTOR Pathway Other Products
ALX-430-096
Revised 24-Feb-05
A77 1726
SYNONYMS
N-(4-Trifluoromethylphenyl)-2-cyano-3-hydroxycrotonamide
2-Cyano-3-hydroxy-N-[4-(trifluoromethyl)phenyl]-2-butenamide
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Tyrosine Kinase Inhibitors
Ordering Information
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ALX-430-096-M005
5 mg
45.00 USD
ALX-430-096-M025
25 mg
180.00 USD
Product Specification
FORMULA:
C
12
H
9
F
3
N
2
O
2
MW:
270.2
CAS NUMBER:
108605-62-5
PURITY:
≥98%
APPEARANCE:
White solid.
SOLUBILITY:
Soluble in DMSO.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
+4°C
HANDLING:
Protect from light. Keep under inert gas.
Product Description
Physiologically active metabolite of the immunosuppressive drug leflunomide (Prod. No.
ALX-430-095
). Inhibits the activity of dihydrorotate dehydrogenase and of protein tyrosine kinases. Blocks TNF-mediated NF-κB activation in a dose- and time-dependent manner. Also inhibits the activity of cyclooxygenase-2 (COX-2)
in vitro
and
in vivo
.
Product Specific Literature References
Inhibition of the epidermal growth factor receptor tyrosine kinase activity by leflunomide:
T. Mattar, et al.; FEBS Lett.
334
, 161 (1993)
Abstract
Inhibition of protein tyrosine phosphorylation in T cells by a novel immunosuppressive agent, leflunomide:
X. Xu, et al.; J. Biol. Chem.
270
, 12398 (1995)
Abstract
;
Full Text
The immunosuppressive metabolite of leflunomide is a potent inhibitor of human dihydroorotate dehydrogenase:
J.P. Davis, et al.; Biochemistry
35
, 1270 (1996)
Abstract
Two activities of the immunosuppressive metabolite of leflunomide, A77 1726. Inhibition of pyrimidine nucleotide synthesis and protein tyrosine phosphorylation:
X. Xu, et al.; Biochem. Pharmacol.
52
, 527 (1996)
Abstract
The immunosuppressive metabolite of leflunomide, A77 1726, affects murine T cells through two biochemical mechanisms:
R.T. Elder, et al.; J. Immunol.
159
, 22 (1997)
Abstract
In vivo mechanism by which leflunomide controls lymphoproliferative and autoimmune disease in MRL/MpJ-lpr/lpr mice:
X. Xu, et al.; J. Immunol.
159
, 167 (1997)
Abstract
Immunosuppressive leflunomide metabolite (A77 1726) blocks TNF-dependent nuclear factor-kappa B activation and gene expression:
S.K. Manna & B.B. Aggarwal; J. Immunol.
162
, 2095 (1999)
Abstract
A771726, the active metabolite of leflunomide, directly inhibits the activity of cyclo-oxygenase-2 in vitro and in vivo in a substrate-sensitive manner:
L.C. Hamilton, et al.; Br. J. Pharmacol.
127
, 1589 (1999)
Abstract
Further Categories Containing This Product:
NF-kB Pathway Inhibitors
•
COX Inhibitors
•
Immunomodulators Other Products
ALX-151-026
Revised 20-Jun-08
N-Acetyl-Asp-Tyr(2-malonyl)-Val-Pro-Met-Leu-NH2
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Tyrosine Kinase Inhibitors
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ALX-151-026-M001
1 mg
90.00 USD
Product Specification
FORMULA:
C
39
H
57
N
7
O
14
S
MW:
880.0
PURITY:
≥96% (HPLC)
APPEARANCE:
White to off-white powder.
SOLUBILITY:
Soluble in water (1mg/ml).
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
USE/STABILITY:
Peptide is very unstable.
Product Description
Peptide containing a phosphotyrosyl mimetic. Effective protein tyrosine kinase inhibitor. Inhibits the phosphoinositide 3-kinase (PI(3)K) C-terminal p85 SH2 domain.
Product Specific Literature References
L-O-(2-malonyl)tyrosine: a new phosphotyrosyl mimetic for the preparation of Src homology 2 domain inhibitory peptides:
B. Ye, et al.; J. Med. Chem.
38
, 4270 (1995)
Abstract
Further Categories Containing This Product:
Peptides
•
Phosphoinositide 3-kinase [PI(3)K] / Related Products
ALX-151-027
Revised 17-Jan-05
N-Acetyl-Asp-Tyr(PO3H2)-Val-Pro-Met-Leu-NH2
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Tyrosine Kinase Inhibitors
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ALX-151-027-M001
1 mg
90.00 USD
Product Specification
FORMULA:
C
36
H
57
N
7
O
13
SP
MW:
858.9
PURITY:
≥96%
SOLUBILITY:
Soluble in water.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
Product Description
Phosphotyrosine containing peptide. Effective protein tyrosine kinase inhibitor. Inhibits the phosphoinositide 3-kinase (PI(3)K) C-terminal p85 SH2 domain.
Product Specific Literature References
L-O-(2-malonyl)tyrosine: a new phosphotyrosyl mimetic for the preparation of Src homology 2 domain inhibitory peptides:
B. Ye, et al.; J. Med. Chem.
38
, 4270 (1995)
Abstract
Further Categories Containing This Product:
Peptides
•
Phosphoinositide 3-kinase [PI(3)K] / Related Products
ALX-350-310
Revised 03-Apr-08
3-O-Acetyl-11-keto-β-boswellic acid
SYNONYMS
AKβBA
PRODUCT LINE
Natural Products / Antibiotics
PRODUCT CATEGORY
Natural Products - Antitumor Reagents
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ALX-350-310-M005
5 mg
130.00 USD
Product Specification
FORMULA:
C
32
H
48
O
5
MW:
512.7
CAS NUMBER:
67416-61-9
SOURCE/HOST:
Isolated from
Boswellia serrata.
PURITY:
≥99% (HPLC, NMR)
APPEARANCE:
White to off-white solid.
SOLUBILITY:
Soluble in acetone, dichloromethane, diethyl ether or DMSO.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
USE/STABILITY:
Stock solutions are stable for up to 3 months when stored at -20°C.
HANDLING:
Protect from light.
HAZARD:
MAY BE CARCINOGENIC. HARMFUL.
Product Description
Shows antitumor and anti-inflammatory activities. Potent non-redox, noncompetitive 5-lipoxygenase and topoisomerase I and IIa inhibitor leading to apoptosis. 10-times more potent than 3-O-acetyl-β-boswellic acid (Prod. No.
ALX-350-308
). Exhibits
in vivo
efficacy in tumor growth and inhibition.
Product Specific Literature References
Acetyl-11-keto-beta-boswellic acid induces apoptosis in HL-60 and CCRF-CEM cells and inhibits topoisomerase I:
R.F. Hoernlein, et al.; J. Pharmacol. Exp. Ther.
288
, 613 (1999)
Abstract
;
Full Text
Boswellic acids activate p42(MAPK) and p38 MAPK and stimulate Ca(2+) mobilization:
A. Altmann, et al.; BBRC
290
, 185 (2002)
Abstract
Coupling of boswellic acid-induced Ca2+ mobilisation and MAPK activation to lipid metabolism and peroxide formation in human leucocytes:
A. Altmann, et al.; Br. J. Pharmacol.
141
, 223 (2004)
Abstract
;
Full Text
Inhibition of IkappaB kinase activity by acetyl-boswellic acids promotes apoptosis in androgen-independent PC-3 prostate cancer cells in vitro and in vivo:
T. Syrovets, et al.; J. Biol. Chem.
280
, 6170 (2005)
Abstract
;
Full Text
Boswellic acids: biological actions and molecular targets:
D. Poeckel & O. Werz; Curr. Med. Chem.
13
, 3359 (2006), Review
Abstract
Mechanisms underlying the anti-inflammatory actions of boswellic acid derivatives in experimental colitis:
C. Anthoni, et al.; Am. J. Physiol. Gastrointest. Liver Physiol.
290
, G1131 (2006)
Abstract
Potentiation of antinociceptive effect of NSAIDs by a specific lipooxygenase inhibitor, acetyl 11-keto-beta boswellic acid:
M. Bishnoi, et al.; Indian J. Exp. Biol.
44
, 128 (2006)
Abstract
Related Products
ALX-350-308
3-O-Acetyl-β-boswellic acid
Further Categories Containing This Product:
Natural Products - Protein Kinase Inhibitors
•
Natural Products - Topoisomerase Inhibitors
•
Lipoxygenases / Related Products
•
NF-kB Pathway Inhibitors
•
Natural Products - Anti-inflammatory Agents
•
Antitumor Agents (Apoptosis Inducers)
•
Natural Products - NF-kB Pathway Inhibitors
•
Natural Products - Apoptosis Inducers & Inhibitors
ALX-480-021
Revised 16-Dec-04
Adenosine 5'-triphosphate . disodium salt
SYNONYMS
ATP . 2Na
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Adenosine Derivatives Other Products
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ALX-480-021-G001
1 g
15.00 USD
ALX-480-021-G005
5 g
45.00 USD
Product Specification
FORMULA:
C
10
H
14
N
5
O
13
P
3
. 2Na
MW:
505.2 . 46.0
CAS NUMBER:
51963-61-2
MERCK INDEX:
14:
155
PURITY:
≥99%
APPEARANCE:
White to off-white powder.
SOLUBILITY:
Soluble in water.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Protect from moisture. Keep cool and dry.
Further Categories Containing This Product:
Inflammasome
ALX-850-323
Revised 31-Jul-08
ADMA Direct (human) ELISA Kit
PRODUCT LINE
Nitric Oxide Pathway
PRODUCT CATEGORY
Nitric Oxide & NOS Detection / Related Products
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ALX-850-323-KI01
1 Kit
1'100.00 USD
Product Specification
SENSITIVITY:
0.05μmol/l (expected value: 0.45µmol/l ± 0.19µmol/l)
QUANTITY:
96 wells (~80 tests).
APPLICATION:
For the quantitative detection of asymmetrical dimethylarginine (ADMA) in human EDTA-plasma and serum. Does not cross-react with SDMA, NMMA or L-arginine.
SHIPPING:
SHIPPED ON BLUE ICE
LONG TERM STORAGE:
+4°C
HANDLING:
Store standard and controls at -20°C. Store rest of the kit at +4°C.
General Information
Asymmetric dimethylarginine (ADMA) is an endogenous inhibitor of nitric oxide (NO) synthesis. NO is one of the major endothelium-derived vasoactive mediators and is involved in the modulation of blood flow and blood pressure. Even small changes of ADMA concentration alter vascular NO production, vascular tone, and systemic vascular resistence. Elevated ADMA concentrations are found in patients with diabetes mellitus, hypercholeste-rolemia, hypertension, pulmonary hypertension, peripheral arterial disease, chronic renal failure, preeclampsia or erectile dysfunction. ADMA is therefore a novel cardiovascular risk factor.
MANUFACTURER
Manufactured by Immundiagnostik AG.
Related Products
ALX-850-327
ADMA Direct (mouse/rat) ELISA Kit
Further Categories Containing This Product:
ELISA & EIA Kits
•
PRMTs, Mono- & Dimethylarginine / Related Products
ALX-850-327
Revised 31-Jul-08
ADMA Direct (mouse/rat) ELISA Kit
PRODUCT LINE
Nitric Oxide Pathway
PRODUCT CATEGORY
Nitric Oxide & NOS Detection / Related Products
Ordering Information
Product Numbers:
Format:
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ALX-850-327-KI01
1 Kit
1'400.00 USD
Product Specification
SENSITIVITY:
0.05μmol/l
QUANTITY:
96 wells (~80 tests).
APPLICATION:
For the quantitative detection of asymmetrical dimethylarginine (ADMA) in mouse or rat EDTA-plasma and serum. Does not cross-react with SDMA, NMMA or L-arginine.
SHIPPING:
SHIPPED ON BLUE ICE
LONG TERM STORAGE:
+4°C
HANDLING:
Store standard and controls at -20°C. Store rest of the kit at +4°C.
General Information
Asymmetric dimethylarginine (ADMA) is an endogenous inhibitor of nitric oxide (NO) synthesis. NO is one of the major endothelium-derived vasoactive mediators and is involved in the modulation of blood flow and blood pressure. Even small changes of ADMA concentration alter vascular NO production, vascular tone, and systemic vascular resistence. Elevated ADMA concentrations are found in patients with diabetes mellitus, hypercholeste-rolemia, hypertension, pulmonary hypertension, peripheral arterial disease, chronic renal failure, preeclampsia or erectile dysfunction. ADMA is therefore a novel cardiovascular risk factor.
MANUFACTURER
Manufactured by Immundiagnostik AG.
Related Products
ALX-850-323
ADMA Direct (human) ELISA Kit
Further Categories Containing This Product:
ELISA & EIA Kits
•
PRMTs, Mono- & Dimethylarginine / Related Products
ALX-270-385
Revised 17-Jul-07
Aloisine A
SYNONYMS
RP107
7-
n
-Butyl-6-(4-hydroxyphenyl)[5
H
]pyrrolo[2,3-
b
]pyrazine
PRODUCT LINE
Cell Cycle
PRODUCT CATEGORY
CDK & Cyclin Inhibitors
Ordering Information
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ALX-270-385-M001
1 mg
30.00 USD
Product Specification
FORMULA:
C
16
H
17
N
3
O
MW:
267.3
PURITY:
≥95%
APPEARANCE:
Yellow solid.
SOLUBILITY:
Soluble in DMSO.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Protect from light. Packaged under inert gas.
Product Description
Cell permeable, potent, selective, reversible and ATP-competitive inhibitor of CDK1/cyclin B (IC
50
=150nM), CDK2/cyclin A (IC
50
=120nM), CDK2/cyclin E (IC
50
=400nM), CDK5/p25
(IC
50
=200nM), CDK5/p35 (IC
50
=160nM) and GSK-3α (IC
50
=500nM). Also inhibits GSK-3β (IC
50
=650nM) and c-Jun N-terminal kinase (JNK) (IC
50
~3-10µM). Poor inhibitor of CK1, CK2, CDK4/cyclin D1, MAPKK, PKA, PKG, PKCs and c-raf (IC
50
≥100µM). Blocks cell cycle in both G1 and G2 phase.
Product Specific Literature References
Aloisines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects
:
Y. Mettey, et al.; J. Med. Chem.
46
, 222 (2003)
Abstract
Further Categories Containing This Product:
GSK-3 Inhibitors
•
JNK [SAPK1] / Related Products
•
Cell Cycle Blockers & Inhibitors / Related Products
ALX-350-270
Revised 08-Feb-08
α-Amanitin